Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2013 Feb 15;23(4):979-84. doi: 10.1016/j.bmcl.2012.12.042. Epub 2012 Dec 21.

Discovery of potent, selective and orally bioavailable imidazo[1,5-a]pyrazine derived ACK1 inhibitors.

Author information

1
OSI Pharmaceuticals, LLC, A Wholly-Owned Subsidiary of Astellas US LLC, 1 Bioscience Park Drive, Farmingdale, NY 11735, USA. Meizhong.jin@astellas.com

Abstract

This Letter describes the medicinal chemistry effort towards a series of novel imidazo[1,5-a]pyrazine derived inhibitors of ACK1. Virtual screening led to the discovery of the initial hit, and subsequent exploration of structure-activity relationships and optimization of drug metabolism and pharmacokinetic properties led to the identification of potent, selective and orally bioavailable ACK1 inhibitors.

PMID:
23317569
DOI:
10.1016/j.bmcl.2012.12.042
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center